Toluene → Bazedoxifene

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene hydrochloride (5 g) and dimethylformamide (50 mL) are charged into a round bottomed flask, heated to 70-75° C. and stirred for clear solution. The reaction mixture is cooled to 25-35° C. followed by addition of triethylamine (2 mL), toluene (150 mL) and water (150 mL) and subsequently the mixture is stirred at room temperature for 5-6 hours. The solid formed is collected by filtration, washed with water (10 mL), toluene (10 mL) and dried under vacuum below 50° C. to afford crystalline bazedoxifene free base Form A of 99.72% HPLC purity.

Provenance & Evidence